专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20100221264A1 Inhibition of HIV-1 Replication by Disruption of the Processing of the Viral Capsid-Spacer Peptide 1 Protein 有权
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US20100221264A1
公开(公告)日：2010-09-02
申请号：US12498157
申请日：2009-07-06
申请人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： A61K39/395 , A61K31/655 , A61K38/16 , A61P31/18 , A61K31/56
CPC分类号： A61K45/06 , A61K31/56 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这样的化合物通过结合Gag蛋白水解切割位点而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

2. 发明申请

US20080233559A1 Inhibition of HIV-1 Replication by Disruption of the Processing of the Viral Capsid-Spacer Peptide 1 Protein 审中-公开
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US20080233559A1
公开(公告)日：2008-09-25
申请号：US11962315
申请日：2007-12-21
申请人： Karl SALZWEDEL , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl SALZWEDEL , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： C12Q1/70
CPC分类号： A61K31/215 , A61K31/56 , A61K31/567 , A61K45/06 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N33/56988 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这些化合物通过结合Gag而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

3. 发明授权

US07537765B2 Inhibition of HIV-1 replication by disruption of the processing of the viral capsid-spacer peptide 1 protein 有权
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US07537765B2
公开(公告)日：2009-05-26
申请号：US10851637
申请日：2004-05-24
申请人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： A61K39/00 , A61K39/12 , A61K39/21 , A61K38/00
CPC分类号： A61K31/215 , A61K31/56 , A61K31/567 , A61K45/06 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N33/56988 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这些化合物通过结合Gag而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

4. 发明申请

US20080200550A1 Inhibition of Hiv-1 Replication by Disruption of the Processing of the Viral Capsid-Spacer Peptide 1 Protein 审中-公开
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工抑制HIF-1复制
公开(公告)号：US20080200550A1
公开(公告)日：2008-08-21
申请号：US11597431
申请日：2005-05-24
申请人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： A61K31/557
CPC分类号： A61K31/215 , A61K31/56 , A61K31/567 , A61K45/06 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N33/56988 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这些化合物通过结合Gag而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

5. 发明授权

US08318425B2 Inhibition of HIV-1 replication by disruption of the processing of the viral capsid-spacer peptide 1 protein 有权
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US08318425B2
公开(公告)日：2012-11-27
申请号：US12498157
申请日：2009-07-06
申请人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： C12Q1/70 , C12Q1/68 , A01N61/00 , A01N57/00 , A61K31/00 , A61K31/66
CPC分类号： A61K45/06 , A61K31/56 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这样的化合物通过结合Gag蛋白水解切割位点而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

6. 发明授权

US07365221B2 Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof 失效
标题翻译：单酰化桦木醇和二氢甜菜蛋白衍生物，其制备及其用途
公开(公告)号：US07365221B2
公开(公告)日：2008-04-29
申请号：US10870555
申请日：2004-06-18
申请人： Graham P. Allaway , Carl T. Wild , Yoshiki Kashiwada , Kuo-Hsiung Lee
发明人： Graham P. Allaway , Carl T. Wild , Yoshiki Kashiwada , Kuo-Hsiung Lee
IPC分类号： C07C69/74
CPC分类号： C07J53/00 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.
摘要翻译：已经发现根据本发明的桦木醇和二氢甜菜碱酰基衍生物具有有效的抗HIV活性。本发明的化合物具有本文所述的式I或其药学上可接受的盐; 其中R 1是C 2 -C 20 - 取代或未取代的羧酰基或其酯; R 2是氢，卤素，羟基或-OR 3，R 3是C 2 -C 3 取代或未取代的羧酰基; 且R 4是氢或C（C 6 H 5）3 N 3。其中虚线表示C20和C29之间任选的双键。

7. 发明授权

US06768007B2 Substituted 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs, compositions thereof, and methods for using thereof 失效
标题翻译：取代的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物，其组合物及其使用方法
公开(公告)号：US06768007B2
公开(公告)日：2004-07-27
申请号：US10096107
申请日：2002-03-13
申请人： Kuo-Hsiung Lee , Lan Xie , Graham P. Allaway , Carl T. Wild
发明人： Kuo-Hsiung Lee , Lan Xie , Graham P. Allaway , Carl T. Wild
IPC分类号： C07D21302
CPC分类号： C07D471/04 , C07D493/04 , C07D495/04 , C07F9/6561
摘要： 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.
摘要翻译：已经发现根据本发明的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物具有抗HIV活性。本发明的化合物具有下式：或其药学上可接受的盐，酯或前药，其中R 1，R 2，R 3，R 4，X和Z被置于规格。本发明还涉及包含一种或多种式I化合物的药物组合物，任选地还包含一种或多种抗病毒剂或免疫刺激剂。此外，本发明涉及式I化合物用于抑制动物细胞或组织中的逆转录病毒感染，用于治疗患有逆转录病毒相关病理学的患者，用于预防HIV传播感染艾滋病毒的孕妇到胎儿的感染，以及在性交期间预防艾滋病毒感染的传播。

8. 发明授权

US06605427B2 Assay for detection of viral fusion inhibitors 失效
公开(公告)号：US06605427B2
公开(公告)日：2003-08-12
申请号：US09779451
申请日：2001-02-09
申请人： Carl T. Wild , Graham P. Allaway
发明人： Carl T. Wild , Graham P. Allaway
IPC分类号： C12Q170
CPC分类号： G01N33/5047 , G01N33/5008 , G01N33/5091 , G01N33/56983 , G01N33/56988 , G01N2333/162 , Y10S977/927 , Y10S977/959
摘要： The invention is directed to a methods for identifying compounds that inhibit or prevent infection of cells by enveloped viruses such as HIV-1 by preventing or disrupting conformational changes in the viral transmembrane protein that are required for virus fusion with those cells, and the compounds discovered by such methods. The invention also includes using these assays as diagnostic assays to detect antibodies in virus infected individuals that inhibit the viral entry processes.

9. 发明授权

US06824783B1 Methods for inhibition of membrane fusion-associated events, including HIV transmission 失效
标题翻译：抑制膜融合相关事件的方法，包括HIV传播
公开(公告)号：US06824783B1
公开(公告)日：2004-11-30
申请号：US08487266
申请日：1995-06-07
申请人： Dani Paul Bolognesi , Thomas James Matthews , Carl T. Wild
发明人： Dani Paul Bolognesi , Thomas James Matthews , Carl T. Wild
IPC分类号： A61K3921
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K2039/525 , A61K2039/555 , A61K2039/60 , A61K2039/6031 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0817 , C07K5/0819 , C07K5/1008 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K14/21 , C07K14/22 , C07K14/245 , C07K14/285 , C07K14/31 , C07K2319/00 , C12N7/00 , C12N2710/16222 , C12N2730/10122 , C12N2740/13022 , C12N2740/14022 , C12N2740/15022 , C12N2740/16122 , C12N2740/16222 , C12N2740/17022 , C12N2760/16122 , C12N2760/18022 , C12N2760/18122 , C12N2760/18422 , C12N2760/18522 , C12N2760/18622 , C12N2760/18722 , G01N33/5008 , G01N33/502 , G01N33/505 , G01N33/5091 , Y10S530/826
摘要： The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.
摘要翻译：本发明涉及显示出有力的抗逆转录病毒活性的肽。本发明的肽包含对应于HIV-1LAI gp41蛋白的氨基酸638至673的DP178（SEQ ID：1）肽，以及DP178的片段，类似物和同系物。本发明还涉及这样的肽的用途，例如抑制人和非人类逆转录病毒，特别是HIV，向未感染细胞的传播。

10. 发明授权

US07122190B2 Fusion proteins comprising DP-178 and other viral fusion inhibitor peptides useful for treating aids 失效
标题翻译：包含DP-178和用于治疗辅助剂的其它病毒融合抑制剂肽的融合蛋白
公开(公告)号：US07122190B2
公开(公告)日：2006-10-17
申请号：US10267748
申请日：2002-10-09
申请人： Dani Paul Bolognesi , Thomas James Matthews , Carl T. Wild , Shawn O'Lin Barney , Dennis Michael Lambert , Stephen Robert Petteway , Alphonse J. Langlois
发明人： Dani Paul Bolognesi , Thomas James Matthews , Carl T. Wild , Shawn O'Lin Barney , Dennis Michael Lambert , Stephen Robert Petteway , Alphonse J. Langlois
IPC分类号： A61K39/21
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K2039/525 , A61K2039/555 , A61K2039/60 , A61K2039/6031 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0817 , C07K5/0819 , C07K5/1008 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K14/21 , C07K14/22 , C07K14/245 , C07K14/285 , C07K14/31 , C07K2319/00 , C12N7/00 , C12N2710/16222 , C12N2730/10122 , C12N2740/13022 , C12N2740/14022 , C12N2740/15022 , C12N2740/16122 , C12N2740/16222 , C12N2740/17022 , C12N2760/16122 , C12N2760/18022 , C12N2760/18122 , C12N2760/18422 , C12N2760/18522 , C12N2760/18622 , C12N2760/18722 , G01N33/5008 , G01N33/502 , G01N33/505 , G01N33/5091 , Y10S530/826
摘要： The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.
摘要翻译：本发明涉及显示出有力的抗逆转录病毒活性的肽。本发明的肽包含对应于HIV-1细胞gp41蛋白的氨基酸638至673的DP178（SEQ ID：1）肽以及DP178的片段，类似物和同系物。本发明还涉及这样的肽的用途，例如抑制人和非人类逆转录病毒，特别是HIV，向未感染细胞的传播。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式